Abstract
Drug discovery and development is a high-risk enterprise that requires significant investments in capital, time and scientific expertise. The studies of xenobiotic metabolism remain as one of the main topics in the research and development of drugs, cosmetics and nutritional supplements.
Antihypertensive drugs are used for the treatment of high blood pressure, which is one the most frequent symptoms of the patients that undergo cardiovascular diseases such as myocardial infraction and strokes. In current cardiovascular disease pharmacology, four drug clusters - Angiotensin Converting Enzyme Inhibitors, Beta-Blockers, Calcium Channel Blockers and Diuretics - cover the major therapeutic characteristics of the most antihypertensive drugs. The pharmacokinetic and specifically the metabolic profile of the antihypertensive agents are intensively studied because of the broad inter-individual variability on plasma concentrations and the diversity on the efficacy response especially due to the P450 dependent metabolic status they present.
Several computational methods have been developed with the aim to: (i) model and better understand the human drug metabolism; and (ii) enhance the experimental investigation of the metabolism of small xenobiotic molecules. The main predictive tools these methods employ are rule-based approaches, quantitative structure metabolism/activity relationships and docking approaches.
This review paper provides detailed metabolic profiles of the major clusters of antihypertensive agents, including their metabolites and their metabolizing enzymes, and it also provides specific information concerning the computational approaches that have been used to predict the metabolic profile of several antihypertensive drugs.
Keywords: Antihypertensive drugs, metabolism, computational approaches.
Current Pharmaceutical Design
Title:Antihypertensive Drugs Metabolism: An Update to Pharmacokinetic Profiles and Computational Approaches
Volume: 21 Issue: 6
Author(s): Aikaterini Zisaki, Ljubisa Miskovic and Vassily Hatzimanikatis
Affiliation:
Keywords: Antihypertensive drugs, metabolism, computational approaches.
Abstract: Drug discovery and development is a high-risk enterprise that requires significant investments in capital, time and scientific expertise. The studies of xenobiotic metabolism remain as one of the main topics in the research and development of drugs, cosmetics and nutritional supplements.
Antihypertensive drugs are used for the treatment of high blood pressure, which is one the most frequent symptoms of the patients that undergo cardiovascular diseases such as myocardial infraction and strokes. In current cardiovascular disease pharmacology, four drug clusters - Angiotensin Converting Enzyme Inhibitors, Beta-Blockers, Calcium Channel Blockers and Diuretics - cover the major therapeutic characteristics of the most antihypertensive drugs. The pharmacokinetic and specifically the metabolic profile of the antihypertensive agents are intensively studied because of the broad inter-individual variability on plasma concentrations and the diversity on the efficacy response especially due to the P450 dependent metabolic status they present.
Several computational methods have been developed with the aim to: (i) model and better understand the human drug metabolism; and (ii) enhance the experimental investigation of the metabolism of small xenobiotic molecules. The main predictive tools these methods employ are rule-based approaches, quantitative structure metabolism/activity relationships and docking approaches.
This review paper provides detailed metabolic profiles of the major clusters of antihypertensive agents, including their metabolites and their metabolizing enzymes, and it also provides specific information concerning the computational approaches that have been used to predict the metabolic profile of several antihypertensive drugs.
Export Options
About this article
Cite this article as:
Zisaki Aikaterini, Miskovic Ljubisa and Hatzimanikatis Vassily, Antihypertensive Drugs Metabolism: An Update to Pharmacokinetic Profiles and Computational Approaches, Current Pharmaceutical Design 2015; 21 (6) . https://dx.doi.org/10.2174/1381612820666141024151119
DOI https://dx.doi.org/10.2174/1381612820666141024151119 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
?Revolutionizing Cancer Treatment: Nano-Therapeutics Targeting Tumor Microenvironment?
This thematic issue explores the forefront of cancer treatment, centering on the groundbreaking potential of nano-therapeutics meticulously designed to target the tumor microenvironment. At its core, the issue aims to unravel the latest advancements in nanotechnology, showcasing innovative materials, formulations, and delivery systems that hold promise for redefining cancer therapeutics. ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Receptor for AGEs (RAGE) as Mediator of NF-kB Pathway Activation in Neuroinflammation and Oxidative Stress
CNS & Neurological Disorders - Drug Targets Advanced Glycation End Products and Cardiovascular Disease
Current Diabetes Reviews The Glomerular Podocyte as a Target of Growth Hormone Action: Implications for the Pathogenesis of Diabetic Nephropathy
Current Diabetes Reviews Efficacy and Cardiovascular Safety of SGLT2 Inhibitors
Current Drug Safety Nephrotonic and Nephroprotective Medicinal Herbs in Traditional Persian Medicine: Review and Assessment of Scientific Evidence
Current Traditional Medicine Renoprotection and Mechanisms of Erythropoietin and Its Derivatives Helix B Surface Peptide in Kidney Injuries
Current Protein & Peptide Science Diabetes and Complications: Cellular Signaling Pathways, Current Understanding and Targeted Therapies
Current Drug Targets Emerging Therapeutic Targets in Regenerative Medicine for the Treatment of Diabetes Mellitus: A Patent Literature Review
Recent Patents on Regenerative Medicine PDE5 Inhibitor Treatment Options for Urologic and Non-Urologic Indications: 2012 Update
Current Pharmaceutical Design Obesity, Metabolic Syndrome and the Risk of Microvascular Complications in Patients with Diabetes mellitus
Current Pharmaceutical Design Retinal Protein O-GlcNAcylation and the Ocular Renin-angiotensin System: Signaling Cross-roads in Diabetic Retinopathy
Current Diabetes Reviews Pharmacology of Rhein and Advancement in the Synthesis of Its Derivatives
Current Traditional Medicine Stroke Subtypes and their Possible Implication in Stroke Prevention Drug Strategies
Current Vascular Pharmacology Leukocyte-Independent Effects of CC-Chemokines on Vascular Remodeling
Current Pharmaceutical Biotechnology Human PON Promoters: From Similarity to Prediction of Polymorphic Positions within Transcription Factor Elements
Mini-Reviews in Medicinal Chemistry Neurodegeneration in the Pathogenesis of Diabetic Retinopathy: Molecular Mechanisms and Therapeutic Implications
Current Medicinal Chemistry Biomarkers of Protein Oxidation in Human Disease
Current Molecular Medicine Advances in Current Diabetes Proteomics: From the Perspectives of Label- free Quantification and Biomarker Selection
Current Drug Targets An Increasing Incidence of Treatment Resistance in Hypertension?
Current Drug Therapy Blood Platelet Reactivity and its Pharmacological Modulation in (People with) Diabetes Mellitus
Current Pharmaceutical Design